400720-32-3

Upstream product

• 895637-44-2 2,2,2-trifluoro-N-(3-nitrobenzyl)acetamide 
• 383-63-1 ethyl trifluoroacetate, 
• 4403-70-7 m-aminobenzylamine 
• 4403-69-4 2-amino-1-benzylamine 

Downstream Products

• 895637-45-3 2,6-Difluoro-N-[3-(3-{2-[(3-{[(trifluoroacetyl)amino]methyl}phenyl)amino]-4-pyrimidinyl}pyrazolo[1,5-a]pyridin-2-yl)phenyl]benzamide 
• 895637-57-7 2,5-Difluoro-N-[3-(3-{2-[(3-{[(trifluoroacetyl)amino]methyl}phenyl)amino]-4-pyrimidinyl}pyrazolo[1,5-a]pyridin-2-yl)phenyl]benzamide 
• 943721-97-9 ({3-[(2,2,2-trifluoro-acetylamino)-methyl]-phenylcarbamoyl}-methyl)-carbamic acid tert-butyl ester 
• 941319-01-3 2,2,2-trifluoro-N-[(3-{[4-(2-{3-[(3-thienylacetyl)amino]phenyl}-pyrazolo[1,5-a]pyridin-3-yl)-2-pyrimidinyl]amino}phenyl)methyl]acetamide 

Relevant academic research and scientific papers

Exploration of the Structural Space in 4(3 H)-Quinazolinone Antibacterials

We report herein the syntheses of 79 derivatives of the 4(3H)-quinazolinones and their structure-activity relationship (SAR) against methicillin-resistant Staphylococcus aureus (MRSA). Twenty one analogs were further evaluated in in vitro assays. Subsequent investigation of the pharmacokinetic properties singled out compound 73 ((E)-3-(5-carboxy-2-fluorophenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one) for further study. The compound synergized with piperacillin-tazobactam (TZP) both in vitro and in vivo in a clinically relevant mouse model of MRSA infection. The TZP combination lacks activity against MRSA, yet it synergized with compound 73 to kill MRSA in a bactericidal manner. The synergy is rationalized by the ability of the quinazolinones to bind to the allosteric site of penicillin-binding protein (PBP)2a, resulting in opening of the active site, whereby the β-lactam antibiotic now is enabled to bind to the active site in its mechanism of action. The combination effectively treats MRSA infection, for which many antibiotics (including TZP) have faced clinical obsolescence.

2-Pyrimidinyl Pyrazolopyridine ErbB Kinase Inhibitors

The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.

2-Pyrimidinyl Pyrazolopyridine Erbb Kinase Inhibitors

The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.

PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA

Disclosed are novel compounds of formula (I) wherein R1, R2, R3 , R4 and A are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders

2-(ARYLOXY)ACETAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS

The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.

AMINE COMPOUNDS

The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.